AZ8838 |
| رقم الكتالوجGC65312 |
AZ8838 هو مضاد جزيء صغير غير ببتيد فعال شفوياً وقويًا وتنافسيًا لـ PAR2 مع pKi يبلغ 6.4 لـ hPAR2
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2100285-41-2
Sample solution is provided at 25 µL, 10mM.
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AZ8838 is a potent, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pKi of 6.4 for hPAR2[1].
AZ8838 binds in an occluded pocket[1].AZ8838 is a potent antagonist against SLIGRL-NH2 in the Ca2+ assay with a pIC50 of 5.70 ± 0.02[1].AZ8838 shows a potency trend when inhibiting IP1 production (pIC50 = 5.84 ± 0.02)[1].AZ8838 attenuates both peptide-induced phosphorylation of ERK1/2 (pIC50 = 5.7 ± 0.1) and β-arrestin-2 recruitment (pIC50 = 6.1 ± 0.1)[1].
AZ8838 (10 mg/kg; p.o.; 2 h prior) is anti-inflammatory in a PAR2 agonist-induced rat paw oedema model[1].
[1]. Kennedy AJ, et al. Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition. Commun Biol. 2020 Dec 17;3(1):782.
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